83602-39-5

中文名称环孢菌素 H

英文名称 Cyclosporin H

CAS 83602-39-5

分子式 C62H111N11O12

分子量 1202.61

MOL 文件 83602-39-5.mol

更新日期 2024/06/12 09:20:52

83602-39-5 结构式

基本信息物理化学性质安全数据常见问题列表

基本信息

中文别名

环孢素H
环胞霉素B
环孢霉素H
环孢菌素 H
环孢菌素杂质H
环孢素H, 来源于小单孢菌
环[L-丙氨酰-D-丙氨酰-N-甲基-L-亮氨酰-N-甲基-L-亮氨酰-N-甲基-L-缬氨酰-3-羟基-N,4-二甲基-L-2-氨基-6-辛烯酰-L-2-氨基丁酰-N-甲基甘氨酰-N-甲基-L-亮氨酰-L-缬氨酰-N-甲基-L-亮氨酰]

英文别名

Sandoz 37-839
CYCLOSPORIN H
Cyclosporin H, >=95%
Cyclosporine IMpurity-H
5-(N-Methyl-D-valine)cyclosporin A
Cyclosporin H, froM MicroMonospora
5-(N-Methyl-D-valine)cyclosporine A
Cyclo[L-alanyl-D-alanyl-N-methyl-L-leucyl-N-methyl-L-leucyl-N-methyl-D-valyl-3-hydroxy-N,4-dimethyl-L-2-amino-6-octenoyl-L-2-aminobutanoyl-N-methylglycyl-N-methyl-L-leucyl-L-valyl-N-methyl-L-leucyl]
Cyclo[L-alanyl-D-alanyl-N-Methyl-L- leucyl-N-Methyl-L-leucyl-N-Methyl-D-valyl-(3R,4R,6E)-6,7-didehydro-3-hydroxy-N,4-diMethyl-L-2-aMinooctanoyl-L-2-aMinobutanoyl-N-Methylglycyl-N-Methyl-L-leucyl-L-valyl-N-Methyl-L-leucyl]

所属类别

生物化工：激动剂抑制剂

物理化学性质

熔点148-151°C

沸点1293.8±65.0 °C(Predicted)

密度1.016±0.06 g/cm3(Predicted)

储存条件-20°C

储存条件-20°C冷冻

溶解度氯仿（微溶）、甲醇（微溶、加热、超声处理）

酸度系数(pKa)13.32±0.70(Predicted)

形态粉末

颜色白色至米色

旋光性 (optical activity)[α]/D -100 to -115°, c = 0.5 in methanol

安全数据

危险性符号(GHS)

GHS07,GHS08

警示词危险

危险性描述H302-H350-H360

防范说明P202-P264-P270-P280-P301+P312-P308+P313

海关编码29420000

常见问题列表

生物活性

Cyclosporin H 是 FPR-1 (甲酰肽受体 1) 的选择性强效抑制剂。Cyclosporin H 是一种病毒转导 (viral transduction) 增强剂，可使人脐带血来源的造血干细胞和祖细胞 (HSPCs) 中慢病毒转导增强 10 倍。Cyclosporin H 与雷帕霉素 (HY-10219) 或前列腺素 E2 (HY-101952) 联合使用时表现出累加效应。Cyclosporin H 缺乏 Cyclosporin A 具有的免疫抑制活性。

体外研究

The cyclic undecapeptide, cyclosporin H, is a potent inhibitor of formyl-Met-Leu-Phe (FMLP)-induced superoxide anion (O2-) formation in human neutrophils. Cyclosporin H inhibits FMLP binding in HL-60 membranes with a K _i of 0.1 μM. Cyclosporin H inhibits activation by FMLP of high affinity GTPase (the enzymatic activity of alpha-subunits of heterotrimeric regulatory guanine nucleotide-binding proteins) in HL-60 membranes with a K _i of 0.79 μM. Cyclosporin H inhibits the stimulatory effects of FMLP on cytosolic Ca ²⁺ concentration ([Ca ²⁺ ]i), O2- formation, and beta-glucuronidase release with K _i values of 0.08, 0.24, and 0.45 μM, respectively.

体内研究

Cyclosporin H (5 mg/kg; i.p.; before LPS or HCl challenge) attenuats lung injury induced by LPS or HCl (a lung injurymodel).